Secondary-stage drug release vaginal administration preparation and preparation method thereof

Abstract

The invention discloses a secondary-stage drug release vaginal administration preparation comprising the following components: an active ingredient immediate release granule and an active ingredient sustained release granule, wherein the active ingredient immediate release granule comprises an acid source granule and an alkali source granule, and the active ingredient sustained release granule includes a wetting agent and an adhesive. The secondary-stage drug release vaginal administration preparation mainly consists of a sustained-release part and an immediate-release part, and the immediate-release part rapidly releases part of a medicine by the principle of effervescence, and can quickly act on a local lesion of vaginal inflammation, and the slow-release part allows a slow-release skeleton to absorb water to swell to form a gel by the effects of the wetting agent, then adsorbed on the mucosa of the inner wall of the vagina to slowly release the medicine so as to achieve the functionof releasing the medicine for a long time, reducing the number of times of administration, and increasing patient compliance.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a novel controlled-release secondary drug-release preparation for vaginal administration and a preparation method thereof. Background technique [0002] Vaginitis is a common gynecological disease, manifested as vulvar and vaginal itching, burning pain, irritation and abnormal discharge. Usually the reason is that changes in the local environment of the vagina (such as acid-base balance disruption) lead to the destruction of the vagina's natural defenses, allowing certain microorganisms and pathogens to invade, and then trigger vaginal inflammation. Clinically common vaginal inflammations include: bacterial vaginosis (22% to 50%), candidal vaginitis (17% to 39%), trichomonas vaginitis (4% to 35%), senile vaginitis , Young female vaginitis. [0003] Conventional administration methods for treating vaginal inflammation include local vaginal administration in addition to oral administratio...

AI Technical Summary

Problems solved by technology

[0004] Vaginal effervescent tablets have the advantages of convenient administration and quick onset of local administration, but there are mainly the following disadvantages: (1) The administration cycle is short, the administration is frequent, and the drug adhesion is not good, so it can only be used before going to bed. Drug excipients are easy to flow out during drug administration, which affects the full play of the drug effect; (2) For some drugs with short half-lives, the frequency of drug administration will be increased, making it inconvenient to use

[0005] Although oily matrix vaginal suppository is convenient to carry and administer, it has the following disadvantages: (1) the storage conditions are harsh, and when the temperature is high, the suppository is easily softened and deformed, which affects the patient's administration and compliance; (2) oily matrix After melting, it is easy to drip from the vaginal opening, contaminating clothes

Water-soluble base vaginal suppositories are easy to carry and administer, but water-soluble bases are easy to absorb moisture, and require high environmental humidity control and water-proof performance of packaging materials during the production process, which increases production and patient medication costs

At the same time, the vaginal suppository is also administered at night before going to bed, and the administration time is limited

[0006] Vaginal gel has the following defects: (1) poor lubricating effect, easy to lose water and mildew, and a large amount of preservatives need to be added in the production process; (2) special drug delivery equipment is required, which increases the cost and is inconvenient to carry; ( 3) It cannot quickly release the drug quickly, and it cannot take effect quickly for severe patients; (4) For vaginal gel administration, the drug is generally loaded into a gel carrier containing a large amount of water, which is not suitable for easily hydrolyzed drugs. Applicable, and the drug storage conditions are strict; (5) Same as the general disadvantages of traditional vaginal administration dosage forms, it needs to be administered before going to bed, and it is not suitable for exercise

However, the drug release of the gel preparation is slow, and there is no function of rapid drug release and onset of action. The in vitro dissolution evaluation only releases 7% of the drug in 4 hours. For some severe patients, the onset time of the drug in this dosage form is defective.

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